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The search for novel heterocyclic compounds with a natural product skeleton as potent enzyme inhibitors against clinical hits is our prime concern in this study. Here, a simple and facile two-step strategy has been designed to synthesize a series of novel coumarin-based dihydropyranochromenes ( 12a - 12m ) in a basic moiety. The synthesized compounds were thus characterized through spectroscopic techniques and screened for inhibition potency against the cytosolic hCA II isoform and β-glucuronidase. Few of these compounds were potent inhibitors of hCA II and β-glucuronidase with varying IC 50 values ranging from 4.55 ± 0.22 to 21.77 ± 3.32 μM and 440.1 ± 1.17 to 971.3 ± 0.05 μM, respectively. Among the stream of synthesized compounds, 12e and 12i were the most potent inhibitors of β-glucuronidase, while 12h , 12i , and 12j showed greater potency against hCA II. In silico docking studies illustrated the significance of substituted groups on the pyranochromene skeleton and binding pattern of these highly potent compounds inside enzyme pockets., Competing Interests: The authors declare no competing financial interest., (© 2022 The Authors. Published by American Chemical Society.)

Fluorenone-based fluorescent and colorimetric sensors 1 and 2 have been developed that displayed selective detection of iodide ions in the presence of interferences. Sensors displayed the fluorescence emission enhancement response toward I - with detection limits of 8.0 and 11.0 nM, respectively, which is accomplished through inhibition of intramolecular charge transfer and C=N isomerization. Excellent sensitivity and unique fluorescence enhancement response of sensors toward I - make them superior because most of the previously reported iodide sensors are based on the fluorescence quenching mechanism and are less sensitive. The sensing potential of sensors toward I - ions was investigated through 1 H NMR titration, dynamic light scattering, Job's plots, and density functional theory analysis. Further, sensors displayed reversible behavior by the alternate addition of I - and Cu 2+ ions that substantiate their role as recyclable sensors for the on-site detection of I - ions. Advantageously, fluorescence enhancement response of sensors was favorably used for fluorescence imaging of I - in live HeLa cells and the design of the logic gate. These sensors were successfully applied in diversified applications such as the preparation of sensors' coated paper strips and the determination of I - ions in blood serum, food, and real water samples., Competing Interests: The authors declare no competing financial interest., (© 2022 The Authors. Published by American Chemical Society.)

Nitroaromatic explosives are a class of compounds that are responsible for various health hazards and terrorist outrages. Among these, sensitive detection of 2,4,6-trinitrophenol (TNP) explosive has always been highly desirable considering public health and national security. In this regard, three fluorene-based conjugated polymers ( CP 1 , CP 2 , and CP 3 ) were synthesized through the Suzuki-Miyaura coupling reaction and were found to be highly sensitive for fluorescence detection of TNP with detection limits of 3.2, 5.7, and 6.1 pM, respectively. Excellent selectivity of CPs toward TNP was attributed to their unique π-π interactions based on fluorescence studies and density functional theory (DFT) calculations. The high sensitivity of CPs to TNP was attributed to the static quenching mechanism based on the photoinduced electron transfer process and was evaluated by fluorescence, UV-visible absorption, dynamic light scattering, Job's plots, the Benesi-Hildebrand plots, and DFT calculations. CPs were also used for colorimetric and real-water sample analysis for the detection of TNP explosive. Meanwhile, sensor-coated test strips were fabricated for on-site detection of TNP, which makes them convenient solid-supported sensors., Competing Interests: The authors declare no competing financial interest., (© 2021 The Authors. Published by American Chemical Society.)